公开(公告)号：CA2350734C

公开(公告)日：2006-10-10

申请号：CA2350734

申请日：1999-11-05

Applicant: BASF AG

Inventor： HOGER THOMAS ,  KOCK MICHAEL ,  LUBISCH WILFRIED

IPC: C07D235/18 ,  A61K20060101 ,  A61K31/10 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/454 ,  A61P20060101 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P13/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07D20060101 ,  C07D209/14 ,  C07D235/04

Abstract: The invention relates to the use of 2-phenyl-benzimidazoles and 2- phenylindoles of general formula (I), wherein A means N or CH, R1 means hydrogen, branched and unbranched C1-C6 alkyl and a C-atom of the alkyl radical can also carry an OR11 or a group R5, R2 means hydrogen, chlorine, fluorine, bromine, iodine, branched and unbranched C1-C6 alkyl, nitro, CF3, CN, NR21R22, NH-CO-R23, OR21, R3 means(CH2)q-NR31R32 and q can be 0, 1, 2 or 3 and R4 means hydrogen, branched and unbranched C1-C6 alkyl, chlorine, bromine, fluorine, nitro, cyano, NR41R42, NH-CO-R43, OR41; as inhibitors of the enzym e poly(ADP-ribose)-polymerase for producing medicaments.

公开(公告)号：NZ514930A

公开(公告)日：2003-10-31

申请号：NZ51493000

申请日：2000-04-11

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOGER THOMAS ,  RANDEL ROLAND ,  SCHULT SABINE ,  MULLER REINHOLD

IPC: C07D235/08 ,  A61K31/4184 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/496 ,  A61K31/551 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D401/08 ,  C07D403/08 ,  C07D2 ,  C07D40

Abstract: Compounds of formula I, or formula II, wherein the variables are defined herein. The compounds are used in the manufacture of medicaments for the treatment of disorders mediated by the inhibition of the enzyme poly(ADP-ribose) polymerase or PARP.

公开(公告)号：TR200101499T1

公开(公告)日：2002-09-23

申请号：TR200101499

申请日：2000-09-15

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOEGER THOMAS ,  SCHULT SABINE ,  GRANDEL ROLAND ,  MUELLER REINHOLD

IPC: A61K31/55 ,  A61P3/10 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  C07D487/06

Abstract: The invention relates to compounds of formula (I) as well as to the tautomeric forms thereof, possible enantiomeric and diastereomeric forms and the prodrugs thereof, the production and use thereof, whereby the values have the meaning as given in the description.

公开(公告)号：SK15952001A3

公开(公告)日：2002-08-06

申请号：SK15952001

申请日：2000-05-03

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  SADOWSKI JENS ,  KOCK MICHAEL ,  HOGER THOMAS

IPC: C07D237/32 ,  A61K31/502 ,  A61P1/10 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/12 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P37/00 ,  A61P41/00 ,  A61P43/00 ,  C07D401/12 ,  C07D403/12 ,  A61K31/00

Abstract: The present invention relates to the use of phthalazine derivatives as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30), to the use as inhibitors of PARP-homologous enzymes and, in particular, these phthalazine derivatives also show a selective inhibition of PARP-homologous enzymes.

公开(公告)号：HK1042084A1

公开(公告)日：2002-08-02

申请号：HK02103400

申请日：2002-05-04

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOGER THOMAS ,  SCHULT SABINE ,  GRANDEL ROLAND ,  MULLER REINHOLD

IPC: A61K20060101 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/496 ,  A61P20060101 ,  A61P3/12 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D235/30 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D ,  A61K ,  A61P

Abstract: Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.

公开(公告)号：BG106056A

公开(公告)日：2002-06-28

申请号：BG10605601

申请日：2001-10-26

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  SADOWSKI JEANS ,  KOCK MICHAEL ,  HOEGER THOMAS

IPC: C07D237/32 ,  A61K31/502 ,  A61P1/10 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/12 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P37/00 ,  A61P41/00 ,  A61P43/00 ,  C07D401/12 ,  C07D403/12 ,  A61K31/00

Abstract: The invention relates to the use of phthalazine derivatives as inhibitors of the enzyme poly(ADP-ribose)polymerase or PARP (EC 2.4.2.30) and to their use as inhibitors of PARP-homologous enzymes. These phthalazine derivatives also exhibit, in particular, a selective inhibition of the PARP-homologous enzymes. 19 claims.

公开(公告)号：ZA200103834B

公开(公告)日：2002-05-13

申请号：ZA200103834

申请日：2001-05-11

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOEGER THOMAS

IPC: C07D235/18 ,  A61K20060101 ,  A61K31/10 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/454 ,  A61P20060101 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P13/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07D20060101 ,  C07D209/14 ,  C07D235/04 ,  C07D ,  A61K ,  A61P

Abstract: 2-Phenylbenzimidazoles and 2-phenylindoles of formula IwhereinA is N or CH,R1 is hydrogen or alkyl which optionally carries an OR11 group,R11 is hydrogen or alkyl,R2 is hydrogen, chlorine, fluorine, bromine, iodine, alkyl, nitro, CF3, CN, NR21R22, NH-CO-R23, OR21,R21 and R22 are each hydrogen or alkyl,R23 is hydrogen, alkyl or phenyl,R3 is -(CH2)q-NR31R32,q is 0, 1, 2 or 3,R31 is hydrogen, alkyl, (CH2)rNR33R34,R32 is (CH2)rNR33R34,r is 2, 3, 4, 5 or 6,R33 and R34 are each hydrogen, alkyl or phenylalkyl wherein the phenyl ring is optionally substituted, orR33 and R34 and the nitrogen atom form a 3- to 8-membered ring,R4 is hydrogen, alkyl, chlorine, bromine, fluorine, nitro, cyano, NR41R42, NH-CO-R43, OR41,R41 and R42 are each hydrogen or alkyl, andR43 is alkyl or phenyl,are useful as inhibitors of poly(ADP-ribose)polymerase and for the production of drugs.

公开(公告)号：BR0010428A

公开(公告)日：2002-04-30

申请号：BR0010428

申请日：2000-05-03

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  SADOWSKI JENS ,  KOCK MICHAEL ,  HOEGER THOMAS

IPC: C07D237/32 ,  A61K31/502 ,  A61P1/10 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/10 ,  A61P25/12 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P37/00 ,  A61P41/00 ,  A61P43/00 ,  C07D401/12 ,  C07D403/12 ,  A61K31/00

Abstract: The present invention relates to the use of phthalazine derivatives as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30), to the use as inhibitors of PARP-homologous enzymes and, in particular, these phthalazine derivatives also show a selective inhibition of PARP-homologous enzymes.

公开(公告)号：BG105018A

公开(公告)日：2001-12-31

申请号：BG10501800

申请日：2000-12-04

Applicant: BASF AG

Inventor： KOCK MICHAEL ,  HOEGER THOMAS ,  KROEGER BURKHARD ,  OTTERBACH BERND ,  LUBISCH WILFRIED ,  LEMAIRE HANS-GEORG

IPC: A01K67/027 ,  A61K38/00 ,  A61K38/45 ,  A61K48/00 ,  A61K49/00 ,  A61P43/00 ,  C07K14/455 ,  C12N1/15 ,  C12N1/19 ,  C12N5/10 ,  C12N9/10 ,  C12N15/09 ,  C12N15/54 ,  C12Q1/68 ,  G01N33/53 ,  A61K31/00

Abstract: The invention relates to poly(ADP-ribose)polymerase (PARP) homologues which are characterised by an amino acid sequence with a) a functional NAD+-binding site, and b) no zinc-finger-sequence motif of general formula CX2CHmHX2C, wherein m is an integral number of 28 or 30 and the radicals X represent any amino acid, independently of each other; and to the functional equivalents of said poly(ADP-ribose)polymerase (PARP) homologues. The invention also relates to nucleic acid coding the poly(ADP-ribose)polymerase (PARP) homologues, to antibodies with specificity for the novel protein, to pharmaceutical and gene therapy agents containing the inventive products, to methods for analytically determining the inventive proteins and nucleic acids, to methods for identifying the effectors or bonding partners of the inventive proteins, to novel PARP effectors and to methods for determining the effectiveness of effectors of this type. 32 claims

公开(公告)号：SK6742001A3

公开(公告)日：2001-12-03

申请号：SK6742001

申请日：1999-11-05

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOGER THOMAS

IPC: C07D235/18 ,  A61K20060101 ,  A61K31/10 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/454 ,  A61P20060101 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P13/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07D20060101 ,  C07D209/14 ,  C07D235/04

Abstract: 2-Phenylbenzimidazoles and 2-phenylindoles of formula IwhereinA is N or CH,R1 is hydrogen or alkyl which optionally carries an OR11 group,R11 is hydrogen or alkyl,R2 is hydrogen, chlorine, fluorine, bromine, iodine, alkyl, nitro, CF3, CN, NR21R22, NH-CO-R23, OR21,R21 and R22 are each hydrogen or alkyl,R23 is hydrogen, alkyl or phenyl,R3 is -(CH2)q-NR31R32,q is 0, 1, 2 or 3,R31 is hydrogen, alkyl, (CH2)rNR33R34,R32 is (CH2)rNR33R34,r is 2, 3, 4, 5 or 6,R33 and R34 are each hydrogen, alkyl or phenylalkyl wherein the phenyl ring is optionally substituted, orR33 and R34 and the nitrogen atom form a 3- to 8-membered ring,R4 is hydrogen, alkyl, chlorine, bromine, fluorine, nitro, cyano, NR41R42, NH-CO-R43, OR41,R41 and R42 are each hydrogen or alkyl, andR43 is alkyl or phenyl,are useful as inhibitors of poly(ADP-ribose)polymerase and for the production of drugs.